Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone (sc-208152). The paullones belong to a family of benzazepinones, and are described to highly inhibit neuronal CDK5/p25 and glycogen synthase kinase-3β (GSK-3β). Studies report that Alsterpaullone activates caspase-9 and enhances apoptosis in Jurkat cells, inhibits CDK5/p25-dependent phosphorylation of DARPP-32 in in vitro mouse striatum slices, and blocks the phosphorylation of Tau by GSK-3β.
1. Leost, M., et al., 2000. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. European journal of biochemistry / FEBS. 267(19): 5983-94. PMID: 10998059
2. Lahusen, Tyler., et al., 2003. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Molecular carcinogenesis. 36(4): 183-94. PMID: 12669310
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PMID: # 10998059
Leost, M. et al. 2000. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur. J. Biochem.. 267: 5983-5994.
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